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公开(公告)号：WO2014137050A1
公开(公告)日：2014-09-12
申请号：PCT/KR2013/008332
申请日：2013-09-16
Applicant: 성균관대학교산학협력단
CPC classification number: A61K41/0028 , A61K9/1676 , A61K47/62 , A61K47/6937
Abstract: 본 발명은 트레일(TRAIL)이 표면 수식되고 화학 항암제가 봉입된 다공성 마이크로입자, 이의 제조방법 및 이의 용도에 관한 것으로, 더욱 상세하게는 폐암의 예방 또는 치료에 있어서 병용투여를 통해 부작용을 줄이고 방출을 조절할 수 있는, 다공성 마이크로입자, 이의 제조방법 및 이의 용도에 관한 것이다.
Abstract translation: 本发明涉及多孔微粒，其中TRAIL是表面改性的，并且引入化学抗癌药物，其制备方法及其用途，更具体地，涉及能够减少副作用并通过伴随给药控制释放的多孔微粒 肺癌预防或治疗，其制备方法及其用途。
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公开(公告)号：KR1020090118879A
公开(公告)日：2009-11-18
申请号：KR1020090042035
申请日：2009-05-14
Applicant: 성균관대학교산학협력단
Abstract: PURPOSE: A PEG-human growth hormone complex is provided to minimize biological activation and last activation in a body. CONSTITUTION: A PEG-human growth hormone complex contains a human growth hormone and polyethyleneglycol(PEG) of 20 kDa-50 kDa. The PEG is methoxyPEG aldehyde(Mpeg-ALD). A pharmaceutical composition for treating dwarfism and growth hormone deficiency or diabetic ulcer contains PEG-human growth hormone complex.
Abstract translation: 目的：提供PEG-人生长激素复合物，以最小化身体中的生物活化和最终活化。 构成：PEG-人生长激素复合物含有20kDa-50kDa的人生长激素和聚乙二醇（PEG）。 PEG是甲氧基-PEG醛（Mpeg-ALD）。 用于治疗侏儒症和生长激素缺乏症或糖尿病性溃疡的药物组合物含有PEG-人生长激素复合物。
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3.发明公开항고지혈, 항산화 및 항바이러스 활성을 갖는 참취추출물로부터 분리된 화합물 失效与HYPOCHESTEROLEMIC，抗氧化和抗病活性相关的CHAMCHI（ASTER SCABER）提取物分离出的具有高磷脂酰肌醇，抗氧化活性和抗病毒活性的化合物
公开(公告)号：KR1020080015769A
公开(公告)日：2008-02-20
申请号：KR1020070137246
申请日：2007-12-26
Applicant: 성균관대학교산학협력단
Abstract: A compound isolated from Aster scaber extracts is provided to ensure excellent hypocholesterolemic, antioxidative, and antiviral actions and be useful for preventing or treating cardiovascular diseases caused by hyperlipidemia and various diseases caused by oxidative stress. A compound isolated from Aster scaber extracts has a structure represented by the following formula 3, 4, or 5. In the formula 3, R is a methyl group, R1 and R3 are caffeoyl groups, and R2 is hydrogen. In the formula 4, R1 and R3 are caffeoyl groups and R2 is hydrogen. In the formula 5, R1 and R3 are hydrogen and R2 is a caffeoyl group. The Aster scaber extracts are obtained by extracting Aster scaber with lower alcohol, and extracting the obtained extract with an organic solvent again. The organic solvent is methanol, methylene chloride, ethylacetate, butanol, or a mixture thereof.
Abstract translation: 提供从Aster scaber提取物分离的化合物，以确保优异的低胆固醇血症，抗氧化和抗病毒作用，并且可用于预防或治疗由高脂血症和由氧化应激引起的各种疾病引起的心血管疾病。 从Aster scaber提取物中分离的化合物具有由下式3,4或5表示的结构。在式3中，R为甲基，R 1和R 3为咖啡酰基，R 2为氢。 在式4中，R1和R3是咖啡酰基，R2是氢。 式5中，R 1和R 3为氢，R 2为咖啡酰基。 通过用低级醇萃取Aster scaber获得Aster scaber提取物，并再次用有机溶剂萃取所得提取物。 有机溶剂是甲醇，二氯甲烷，乙酸乙酯，丁醇或其混合物。
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4.发明授权
公开(公告)号：KR101095396B1
公开(公告)日：2011-12-16
申请号：KR1020090088126
申请日：2009-09-17
Applicant: 성균관대학교산학협력단
Abstract: 본 발명은 천연 트레일 (Tumor Necrosis Factor Related Apoptosis Inducing Ligand, TRAIL)과 동등 또는 유사한 약리활성을 나타내며 약물의 암표적성, 체내 반감기 및 안정성을 증가시킨 트랜스페린-PEG-트레일 결합체 및 결합체의 제조방법에 관한 것이다. 이러한 수용성 고분자가 수식된 트레일은 천연 트레일에 비하여 증가된 암표적성, 우수한 용해도 및 용액 안정성, 그리고 매우 향상된 형태의 약물 동력학적 거동을 보이며, 다양한 종류의 암의 효율적인 치료 및 완화에 유용하게 사용될 수 있다.
트레일, 트랜스페린, PEG, 수용성고분자, 항암 효능, 암표적성-
5.发明公开
公开(公告)号：KR1020110030135A
公开(公告)日：2011-03-23
申请号：KR1020090088126
申请日：2009-09-17
Applicant: 성균관대학교산학협력단
Abstract: PURPOSE: A method for manufacturing transferring-PEG-TRAIL complex is provided to ensure same or similar pharmacological activity and to enhance stability of drug. CONSTITUTION: A transferrin-PEG-TRAIL complex is obtained by binding N-terminal-specific transferring-PEG. The transferring is an AP-transferrin. The trail is a human TRAIL having 281 amino acid sequences. The TRAIL has an isoleucine zipper at the N-terminal. A method for preparing the complex comprises: a step of reacting transferring and PEG or transferring or PEG derivative under the presence of a reductant to shythesize transferring-PEG-aldehyde or transferrrin-PEG derivative-aldehyde complex; and a step of reducing the complex under the presence of reductant.
Abstract translation: 目的：提供转移PEG-TRAIL复合物的制备方法，以确保相同或相似的药理活性并增强药物的稳定性。 构成：通过结合N-末端特异性转移-PEG获得转铁蛋白-PEG-TRAIL复合物。 转移是AP-转铁蛋白。 尾迹是具有281个氨基酸序列的人TRAIL。 TRAIL在N末端有一个异亮氨酸拉链。 制备复合物的方法包括：在还原剂存在下使转移和PEG或转移或PEG衍生物反应以对转移的PEG-醛或转铁蛋白-PEG衍生物 - 醛复合物进行洗脱的步骤; 以及在还原剂存在下还原络合物的步骤。
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Patent Agency Ranking
公开(公告)号：KR100886783B1
公开(公告)日：2009-03-04
申请号：KR1020060052702
申请日：2006-06-12
Applicant: 성균관대학교산학협력단 , 주식회사 넥스엔텍
IPC: A61K47/48
CPC classification number: A61K47/48215 , A61K38/19 , A61K38/191 , A61K47/60 , B01D15/361 , C07K14/52 , C07K14/525 , C07K14/70575 , C07K2319/73 , G01N30/96
Abstract: 본 발명은 N-말단이 수식된 PEG-TRAIL 결합체, 이의 제조방법 및 이의 용도에 관한 것으로서, 보다 구체적으로는 천연 TRAIL(
T umor Necrosis Factor
R elated
A poptosis
I nducing
L igand, TRAIL)과 동등 또는 유사한 약리활성을 나타내며 약물의 체내 반감기 및 안정성을 증가시킨 N-말단이 수식된 PEG-TRAIL 결합체에 관한 것이다. 본 발명의 N-말단이 수식된 PEG-TRAIL 결합체는 천연 TRAIL에 비하여 우수한 용해도 및 용액 안정성, 그리고 매우 향상된 약물 동력학적 거동을 보이며, 증식성 질환 및 자가면역 질환 등의 예방 및 치료에 유용하게 사용될 수 있다.
TRAIL, 폴리에틸렌 글리콜, 수용성고분자, 증식성 질환, 자가면역 질환-
公开(公告)号：KR1020070118492A
公开(公告)日：2007-12-17
申请号：KR1020060052702
申请日：2006-06-12
Applicant: 성균관대학교산학협력단 , 주식회사 넥스엔텍
IPC: A61K47/48
CPC classification number: A61K47/48215 , A61K38/19 , A61K38/191 , A61K47/60 , B01D15/361 , C07K14/52 , C07K14/525 , C07K14/70575 , C07K2319/73 , G01N30/96 , A61K47/50
Abstract: A N-terminal modified PEG(polyethylene glycol)-TRAIL(tumor necrosis factor related apoptosis inducing ligand) is provided to reduce liver toxicity, increase the in vivo retention time, and enhance solubility and stability in solution and pharmacokinetic profiles of TRAIL, so that it is useful for prevention and treatment of proliferative disease and autoimmune disease. A N-terminal modified PEG-TRAIL having non-toxicity to the liver is prepared by linking PEG or PEG derivatives specifically to the N-terminal of TRAIL, wherein PEG is selected from methoxy polyethylene glycol succinimidyl propionate, methoxy polyethylene glycol N-hydroxysuccinimide, methoxy polyethylene glycol aldehyde, methoxy polyethylene glycol maleimide and multi-branched type polyethylene glycol, and the TRAIL contains a zipper amino acid array inducing trimer formation or a terminal group for facilitating the separation and purification.
Abstract translation: 提供N-末端修饰的PEG（聚乙二醇）-TRAIL（肿瘤坏死因子相关的凋亡诱导配体），以减少肝毒性，增加体内保留时间，增强溶液中的溶解度和稳定性以及TRAIL的药代动力学特征，使得 它可用于预防和治疗增殖性疾病和自身免疫性疾病。 通过将PEG或PEG衍生物与TRAIL的N-末端特异性连接，制备具有对肝脏无毒性的N-末端修饰的PEG-TRAIL，其中PEG选自甲氧基聚乙二醇琥珀酰亚胺基丙酸酯，甲氧基聚乙二醇N-羟基琥珀酰亚胺， 甲氧基聚乙二醇醛，甲氧基聚乙二醇马来酰亚胺和多支链型聚乙二醇，TRAIL含有诱导三聚体形成的拉链氨基酸阵列或用于促进分离和纯化的末端基团。
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8.发明授权
公开(公告)号：KR100778633B1
公开(公告)日：2007-11-28
申请号：KR1020070036246
申请日：2007-04-13
Applicant: 성균관대학교산학협력단
IPC: C07D495/04 , A61K31/4188
Abstract: A biotin and biotin polyethylene glycol-linked GLP-1 derivative is provided to be usefully used for preventing or treating diseases caused by excessive secretion of insulin, lowering of glucose in plasma, inhibition of stomach or intestine motion, inhibition of an empty stomach or intestine, or inhibition of food intake, type 2 diabetes, obesity and irritable colon syndrome. A GLP-1 derivative in which biotin and biotin-polyethylene glycol are selectively linked to No. 26 lysine residue and No. 34 lysine residue is represented by the formula(2), wherein the biotin-polyethylene glycol is represented by the formula(1) having a molecular weight of 3,400. A method for preparing the GLP-1 derivative comprises the steps of: (a) adding biotin, biotin-polyethylene glycol and GLP to a buffer solution and an organic solvent to be subject to reaction; (b) storing the reaction mixture obtained from the step(a) under a certain temperature for a certain period of time; (c) removing non-reacted reaction products after the reaction completion of the step(b); and (d) isolating GLP-1 in which the biotin and biotin-polyethylene glycol are linked from the non-reacted products-removed products and purifying them. A pharmaceutical composition for preventing or treating diabetes or obesity comprises the biotin and biotin polyethylene glycol-linked GLP-1 derivative.
Abstract translation: 提供生物素和生物素聚乙二醇连接的GLP-1衍生物可用于预防或治疗由胰岛素过量分泌引起的疾病，血浆中葡萄糖降低，抑制胃或肠运动，抑制空腹或肠 ，或抑制食物摄入，2型糖尿病，肥胖症和肠易激综合征。 生物素和生物素 - 聚乙二醇与26号赖氨酸残基和34号赖氨酸残基选择性连接的GLP-1衍生物由式（2）表示，其中生物素 - 聚乙二醇由式（1 ），分子量为3400。 制备GLP-1衍生物的方法包括以下步骤：（a）将生物素，生物素 - 聚乙二醇和GLP加入缓冲溶液和有机溶剂进行反应; （b）将从步骤（a）获得的反应混合物在一定温度下储存一定时间; （c）在步骤（b）的反应完成后除去未反应的反应产物; 和（d）分离其中生物素和生物素 - 聚乙二醇与未反应的产物去除产物连接的GLP-1并纯化。 用于预防或治疗糖尿病或肥胖症的药物组合物包括生物素和生物素聚乙二醇连接的GLP-1衍生物。
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公开(公告)号：KR1020140109027A
公开(公告)日：2014-09-15
申请号：KR1020130023140
申请日：2013-03-05
Applicant: 성균관대학교산학협력단
CPC classification number: A61K41/0028 , A61K9/1676 , A61K47/62 , A61K47/6937 , A61K9/16 , A61K9/14 , A61K47/30 , A61K47/50
Abstract: The present invention relates to porous microparticles in which the trail is surface modified and a chemical anticancer drug is incorporated, and a preparation method thereof, and more specifically, to porous microparticles capable of reducing side effects and controlling release through concomitant administration in preventing or treating lung cancer, and to a preparation method thereof.
Abstract translation: 本发明涉及多孔微粒，其中轨迹被表面改性，并掺入化学抗癌药物及其制备方法，更具体地说，涉及能够减少副作用的多孔微粒和通过并用给药预防或治疗的多孔微粒 肺癌及其制备方法。
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公开(公告)号：KR1020110007362A
公开(公告)日：2011-01-24
申请号：KR1020090064852
申请日：2009-07-16
Applicant: 성균관대학교산학협력단
CPC classification number: A61K47/34 , Y10S514/866 , Y10S514/909
Abstract: PURPOSE: A pharmaceutical composition for the nasal administration of exedin is provided to improve bioavailability and to treat diseases caused by the suppression of bowel movements or gastric mobility. CONSTITUTION: A pharmaceutical composition for the nasal administration of exedin contains polyethylene glycol or natural or recombinant exedin as a derivative of polyethylene glycol. The exedin is exedin 4. The polyethylene glycol derivative is denoted by chemical formula 1. A therapeutic agent for preventing and treating diabetes, obesity or irritable bowel syndrome contains the pharmaceutical composition.
Abstract translation: 目的：提供用于鼻内施用前列腺素的药物组合物，以改善生物利用度，并治疗由排便或胃移动抑制引起的疾病。 构成：用于鼻内施用前列腺素的药物组合物含有聚乙二醇或作为聚乙二醇衍生物的天然或重组外显子。 前列腺素是exedin 4.聚乙二醇衍生物由化学式1表示。用于预防和治疗糖尿病，肥胖或肠易激综合征的治疗剂含有药物组合物。
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